Key Laboratory of Marine Drugs, Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, PR China.
Carbohydr Res. 2013 Nov 15;381:74-82. doi: 10.1016/j.carres.2013.08.010. Epub 2013 Aug 23.
Eight new aminomannoglycerolipids (2a-h) with linear, branched, or aromatic acyl chains were synthesized and evaluated for their anti-influenza A virus (IAV) activity. By comparing six mannosyl donors with different protecting and leaving groups, the critical glycosylation reaction employed mannosyl trichloroacetimidate with 2-O-benzoyl protecting group as the donor to give the glycoside with absolute α-anomeric selectivity. The bioactivity results showed that the branched compound 2g could effectively inhibit IAV multiplication in MDCK cells with IC50 69.9μM.
八种新的氨基甘露糖甘油脂质（2a-h）具有线性、支链或芳香酰基链，被合成并评估其抗流感 A 病毒（IAV）活性。通过比较六种具有不同保护和离去基团的甘露糖供体，所采用的关键糖基化反应使用带有 2-O-苯甲酰基保护基团的甘露糖三氯乙酰亚胺作为供体，以给出具有绝对α-构型选择性的糖苷。生物活性结果表明，支链化合物 2g 能有效抑制 MDCK 细胞中 IAV 的增殖，IC50 为 69.9μM。
